Abstract
Objective: The aim of the present study was to assess whether quercetin exhibited any inhibitory effect on P-glycoprotein (P-gp)-mediated drug disposition in humans using fexofenadine as a P-gp substrate. Methods: Twelve healthy subjects were enrolled in the study and treated daily for 7 days with 500 mg quercetin or placebo 3 times a day. On day 7, a single dose of 60 mg fexofenadine was administered orally. Plasma and urinary fexofenadine concentrations were measured, and pharmacokinetic differences between placebo and quercetin phases were assessed. Results: The mean plasma concentrations of fexofenadine were significantly increased after quercetin treatment compared to those of the placebo phase. The area under the time versus concentration curve (AUC) of plasma fexofenadine was increased by 55% by quercetin (2,005.3 versus 3,098.6 ng·h/mL, P<0.001) and similarly the maximum plasma concentration (Cmax) during the quercetin phase was elevated by 68% compared to that of the placebo phase (295.3 versus 480.3 ng/mL, P =0.006). Although the oral clearance of fexofenadine was decreased significantly by 37% after quercetin treatment (61.4 versus 38.7 L/h, P<0.001), no differences in the renal clearance and half-life were observed between placebo and quercetin phases. Conclusion: The results of the present study showed that short-term use of quercetin elevated the plasma concentrations of fexofenadine, probably by the inhibition of P-gp-mediated efflux in humans.
| Original language | English |
|---|---|
| Pages (from-to) | 609-614 |
| Number of pages | 6 |
| Journal | European Journal of Clinical Pharmacology |
| Volume | 65 |
| Issue number | 6 |
| DOIs | |
| Publication status | Published - 2009 Jun 1 |
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Keywords
- Drug interaction
- Fexofenadine
- P-glycoprotein
- Quercetin
ASJC Scopus subject areas
- Pharmacology
- Pharmacology (medical)
Cite this
Short-term effect of quercetin on the pharmacokinetics of fexofenadine, a substrate of P-glycoprotein, in healthy volunteers. / Kim, Kyoung Ah; Park, Pil Whan; Park, Ji-Young.
In: European Journal of Clinical Pharmacology, Vol. 65, No. 6, 01.06.2009, p. 609-614.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Short-term effect of quercetin on the pharmacokinetics of fexofenadine, a substrate of P-glycoprotein, in healthy volunteers
AU - Kim, Kyoung Ah
AU - Park, Pil Whan
AU - Park, Ji-Young
PY - 2009/6/1
Y1 - 2009/6/1
N2 - Objective: The aim of the present study was to assess whether quercetin exhibited any inhibitory effect on P-glycoprotein (P-gp)-mediated drug disposition in humans using fexofenadine as a P-gp substrate. Methods: Twelve healthy subjects were enrolled in the study and treated daily for 7 days with 500 mg quercetin or placebo 3 times a day. On day 7, a single dose of 60 mg fexofenadine was administered orally. Plasma and urinary fexofenadine concentrations were measured, and pharmacokinetic differences between placebo and quercetin phases were assessed. Results: The mean plasma concentrations of fexofenadine were significantly increased after quercetin treatment compared to those of the placebo phase. The area under the time versus concentration curve (AUC) of plasma fexofenadine was increased by 55% by quercetin (2,005.3 versus 3,098.6 ng·h/mL, P<0.001) and similarly the maximum plasma concentration (Cmax) during the quercetin phase was elevated by 68% compared to that of the placebo phase (295.3 versus 480.3 ng/mL, P =0.006). Although the oral clearance of fexofenadine was decreased significantly by 37% after quercetin treatment (61.4 versus 38.7 L/h, P<0.001), no differences in the renal clearance and half-life were observed between placebo and quercetin phases. Conclusion: The results of the present study showed that short-term use of quercetin elevated the plasma concentrations of fexofenadine, probably by the inhibition of P-gp-mediated efflux in humans.
AB - Objective: The aim of the present study was to assess whether quercetin exhibited any inhibitory effect on P-glycoprotein (P-gp)-mediated drug disposition in humans using fexofenadine as a P-gp substrate. Methods: Twelve healthy subjects were enrolled in the study and treated daily for 7 days with 500 mg quercetin or placebo 3 times a day. On day 7, a single dose of 60 mg fexofenadine was administered orally. Plasma and urinary fexofenadine concentrations were measured, and pharmacokinetic differences between placebo and quercetin phases were assessed. Results: The mean plasma concentrations of fexofenadine were significantly increased after quercetin treatment compared to those of the placebo phase. The area under the time versus concentration curve (AUC) of plasma fexofenadine was increased by 55% by quercetin (2,005.3 versus 3,098.6 ng·h/mL, P<0.001) and similarly the maximum plasma concentration (Cmax) during the quercetin phase was elevated by 68% compared to that of the placebo phase (295.3 versus 480.3 ng/mL, P =0.006). Although the oral clearance of fexofenadine was decreased significantly by 37% after quercetin treatment (61.4 versus 38.7 L/h, P<0.001), no differences in the renal clearance and half-life were observed between placebo and quercetin phases. Conclusion: The results of the present study showed that short-term use of quercetin elevated the plasma concentrations of fexofenadine, probably by the inhibition of P-gp-mediated efflux in humans.
KW - Drug interaction
KW - Fexofenadine
KW - P-glycoprotein
KW - Quercetin
UR - http://www.scopus.com/inward/record.url?scp=68849107630&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=68849107630&partnerID=8YFLogxK
U2 - 10.1007/s00228-009-0627-6
DO - 10.1007/s00228-009-0627-6
M3 - Article
C2 - 19221726
AN - SCOPUS:68849107630
VL - 65
SP - 609
EP - 614
JO - European Journal of Clinical Pharmacology
JF - European Journal of Clinical Pharmacology
SN - 0031-6970
IS - 6
ER -